Generic
Caffeine Citrate
1 brands available in the market
At a glance
Caffeine Citrate is a methylxanthine medication used in the treatment of apnea of prematurity in premature infants. It stimulates the central nervous system and activates the respiratory center to regulate breathing.
Description
Caffeine Citrate is a methylxanthine structurally related to theophylline and theobromine. It is a bronchial smooth muscle relaxant, a CNS stimulant, a cardiac muscle stimulant, and a diuretic.
The mechanism of action of caffeine in apnea of prematurity is not fully understood, but several mechanisms have been hypothesized: stimulation of the respiratory center, increased minute ventilation, decreased threshold to hypercapnia, increased response to hypercapnia, increased skeletal muscle tone, decreased diaphragmatic fatigue, increased metabolic rate, and increased oxygen consumption. Most of these effects have been attributed to antagonism of adenosine receptors (A1 and A2 subtypes) by caffeine.
Indications
- Apnea of prematurity
Therapeutic class
Painkiller Muscle Relaxant
Pharmacological class
Methylxanthine (Respiratory Stimulant)
Pharmacology
Caffeine Citrate is a methylxanthine that acts as an adenosine receptor antagonist. It stimulates the central nervous system, activates the respiratory center, increases minute ventilation, and reduces diaphragmatic fatigue. In apnea of prematurity, it increases respiratory rate and depth, reducing the frequency of apneic episodes.
Mechanism of action
Caffeine Citrate blocks adenosine receptors (A1 and A2), stimulating the central nervous system, increasing respiratory center sensitivity, and improving diaphragmatic contractility to prevent and treat apnea in premature infants.
Dosage
Loading Dose: 20 mg/kg (Caffeine Citrate), IV infusion (over 30 minutes) using a syringe infusion pump. Frequency: Once.
Maintenance Dose: 5 mg/kg (Caffeine Citrate), IV infusion (over 10 minutes) using a syringe infusion pump. Frequency: Every 24 hours (beginning 24 hours after the loading dose).
Treatment duration: Limited to 10-12 days in clinical trials; long-term safety and efficacy have not been established.
Note: Discard vials containing visible particulate matter. For single use only; discard any unused solution.
Administration
For IV infusion only. Infuse slowly using a syringe infusion pump (Loading: 30 minutes, Maintenance: 10 minutes). Administered by trained healthcare professionals in the Neonatal Intensive Care Unit (NICU).
Missed dose
Hospital-only medicine. Administered by doctor or nurse. Missed dose concept does not apply (hospital-administered).
Side effects
Rare side effects: Sepsis, hemorrhage, necrotizing enterocolitis, gastritis, gastrointestinal hemorrhage, acidosis, cerebral hemorrhage, dyspnea, lung edema, dry skin, rash, skin breakdown, kidney failure.
Overdose symptoms (serum levels >50 mg/L): Fever, tachypnea, insomnia, tremor, hypertonia, seizures, vomiting, hyperglycemia, elevated BUN, elevated total leukocyte concentration.
Precautions & warnings
- For use only in the Neonatal Intensive Care Unit (NICU) by trained healthcare professionals.
- Use with caution in infants with seizure disorders, cardiovascular disease, and impaired renal or hepatic function.
- Monitor serum caffeine concentrations and adjust dose to avoid toxicity.
- Mothers of infants receiving Caffeine Citrate should avoid caffeine-containing foods, beverages, or medicinal products (caffeine is excreted into breast milk).
Contraindications
No known contraindications.
Drug interactions
- Cimetidine and ketoconazole (decrease caffeine elimination): Lower doses may be needed.
- Phenobarbital and phenytoin (increase caffeine elimination): Higher doses may be needed.
- Inter-conversion with theophylline: Inter-conversion between caffeine and theophylline has been reported in preterm neonates; concurrent use is not recommended.
Food interactions
No food-related restrictions (parenteral administration). However, mothers of infants receiving treatment should avoid caffeine-containing foods/beverages (caffeine is excreted into breast milk).
Use in pregnancy
May be unsafe during pregnancy (Category C). Animal studies have shown harmful effects on the developing baby. Use only if clearly needed.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Caffeine is excreted into breast milk. Mothers of newborn infants treated with Caffeine Citrate should not ingest caffeine-containing foods, beverages, or medicinal products containing caffeine.
Pediatric use
Indicated for use in neonates (premature infants). Safety and efficacy in older children have not been established.
Geriatric use
Not for use in elderly patients.
Renal / hepatic impairment
Overdose effects
Serious toxicity has been associated with serum levels >50 mg/L. Signs and symptoms: Fever, tachypnea, insomnia, tremor, hypertonia, seizures, vomiting, hyperglycemia, elevated BUN, elevated total leukocyte concentration. Exchange transfusions may decrease caffeine levels. Seizures may be treated with IV diazepam or pentobarbital sodium.
Storage conditions
Do not store above 30°C. Keep away from light. Keep out of reach of children.
Chemical structure
Caffeine Citrate